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Antimicrob Agents Chemother. 1977 February; 11(2): 198-201
Copyright © 1977 American Society for Microbiology. All Rights Reserved.

Comparative Study of the Antiviral Activity of Acyl Derivatives of 2,2'-Anhydro-1-ß-D-Arabinofuranosylcytosine and Other Nucleosides Against Encephalitis in Mice¹

Shionogi Research Laboratory, Shionogi & Co., Ltd., Fukushima-ku, Osaka, 553 Japan
Institute of Molecular Biology, Syntex Research, Palo Alto, California 94304

ABSTRACT

Anti-deoxyribonucleic acid virus activities of 3'-O-acyl derivatives of 2,2'-anhydro-1-ß-D-arabinofuranosyl cytosine (cyclo-C) and 1-ß-D-arabinofuranosylcytosine (Ara-C) were evaluated by using an in vivo test system in mice. Among the derivatives tested, 3'-O-decanoyl cyclo-C hydrochloride was the most effective against herpes simplex virus-induced encephalitis in mice when the drug was administered directly into infected brains of mice (target-organ treatment). A comparative study of the treatment of herpetic encephalitis in mice with 3'O-decanoyl cyclo-C and other nucleosides, including Ara-C, 9-ß-D-arabinofuranosyladenine (Ara-A), and 5-iodo-2'-deoxyrudine (IUdR), proved Ara-A to be more efficacious than the other nucleosides, followed by 3'-O-decanoyl cyclo-C, which was more active than Ara-C and IUdR. Administration of 3'-O-acyl cyclo-C's by intraperitoneal injection, however, failed to demonstrate activity against herpetic encephalitis in mice. The antivaccinial activity of 3'-O-decanoyl cyclo-C was also compared with that of other compounds against encephalitis and dermal tail lesions in mice caused by vaccinia virus infection. Interaperitoneally administered 3'-O-decanoyl cyclo-C and Ara-C also showed no significant activity against the diseases. Under these test conditions, N-methylisatin-ß-thiosemicarbazone (Marboran) was the most active compound, followed by Ara-A.

¹ Contribution no. 130 from the Institute of Molecular Biology, Syntex Research, Palo Alto, CA 94304.